AR015500A1 - 11 BETA-HALOGEN-STRATRIENS REPLACED IN 7 ALPHA, PROCEDURE FOR PREPARING PHARMACEUTICAL PREPARATIONS THAT CONTAIN SUCH 11 BETA-HALOGEN-STRATRIENS REPLACED IN 7 ALPHA, AS WELL AS USED IN THE PREPARATION OF MEDICINES. - Google Patents
11 BETA-HALOGEN-STRATRIENS REPLACED IN 7 ALPHA, PROCEDURE FOR PREPARING PHARMACEUTICAL PREPARATIONS THAT CONTAIN SUCH 11 BETA-HALOGEN-STRATRIENS REPLACED IN 7 ALPHA, AS WELL AS USED IN THE PREPARATION OF MEDICINES.Info
- Publication number
- AR015500A1 AR015500A1 ARP980106471A ARP980106471A AR015500A1 AR 015500 A1 AR015500 A1 AR 015500A1 AR P980106471 A ARP980106471 A AR P980106471A AR P980106471 A ARP980106471 A AR P980106471A AR 015500 A1 AR015500 A1 AR 015500A1
- Authority
- AR
- Argentina
- Prior art keywords
- carbon atoms
- alkenyl
- branched
- beta
- alpha
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
- C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
- C07J41/0094—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 containing nitrile radicals, including thiocyanide radicals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
- A61P5/30—Oestrogens
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
- A61P5/32—Antioestrogens
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J31/00—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
- C07J31/006—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring not covered by C07J31/003
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
- C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
- C07J41/0072—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 the A ring of the steroid being aromatic
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J43/00—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
- C07J43/003—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton not condensed
Abstract
11 beta-halogeno-estratrienos sustituidos en 7 alfa, de formula I en donde R3 representa un átomo de hidrogeno, un resto de hidrocarburo con hasta 8 átomosde carbono o un resto de la subformula R3 - C(O)-, donde R3 representa un átomo de hidrogeno oun resto de hidrocarburo con hasta 8 átomos de carbono o unresto fenilo, R7 representa un resto con la formula -A-B-Z-R20, donde A figura un enlace directo o un resto bencilideno, donde el grupo metileno está enlazadoal átomo de carbono 7 delesteroi de, o un resto fenilo, Bfigura para un grupo alquileno, alquenilo o alquinilo con 3 a 14 átomos de carbono, lineal oramificado; y Z figura para un grupo -NR21, y R21 para un grupo alquilo C1-3, donde , entonces R20 representa un átomo dehidrogeno, u n grupo alquilo,alquenilo o alquinilo con hasta 10 átomos de carbono, lineal o ramificado, o uno de los agrupamientos D-CnF2n + 1, donde D representa un grupo alquileno,alquenilo o alquinilo con hasta 8 átomos de carbono, lineal oramificado, y n un numero entero de 1 a 8, L-CH = CF - CpF2p + 1, donde L representa un grupoalquileno, alquenilo o alquinilo con C2-7, lineal o ramificado, y representa un numero entero de 2 a 7, D-O-(CH2)-q-arilo, donde D representa lo mismo queloya indicado, q a 0, 1, 2 o 3 y arilo figura para un resto fenilo o 1- o 2-naftilo, en casos dados, sustituido una o dos veces, o un resto heteroarilo,D-O-(CH2)r-CnF2n + 1, donde D y n representan lo mismo que lo ya indicado, y r figura para unnumero entero de 1 a 5, o R20 y R21, junto con el nitrogeno alque están unidos, forman un heterociclo saturado o insaturado con 5 o 6 miembros de cadena que, en casos dados, contiene uno o dos heteroátomos seleccionadosentre nitrogeno, oxígeno yazufre y en casos dados, es ta sustituido o Z figura para -SOx- y x para 0, 1 o 2, donde, entonces, R20 representa un grupo alquilo,alquenilo o alquinilo con hasta 10 átomos de carbono, lineal o ramificado, o uno de los agrupamientos D-CnF2n + 1,donde D representa un grupo alq uileno,alquenilo o alquinilo con hasta 8 átomos de carbono, lineal o ramificado, y n un numero entero de 1 a 8, L - CH = CF - CpF2p + 1, donde L representa un11 beta-halogen-estratriennes substituted in 7 alpha, of formula I wherein R3 represents a hydrogen atom, a hydrocarbon residue with up to 8 carbon atoms or a remainder of the subformula R3-C (O) -, where R3 represents a hydrogen atom or a hydrocarbon residue with up to 8 carbon atoms or a phenyl residue, R7 represents a residue with the formula -ABZ-R20, where A contains a direct bond or a benzylidene residue, where the methylene group is linked to the carbon atom 7 delesteroi of, or a phenyl moiety, Bfigura for an alkylene, alkenyl or alkynyl group with 3 to 14 carbon atoms, linearly branched; and Z is for a group -NR21, and R21 for a C1-3 alkyl group, where, then R20 represents a hydrogen atom, an alkyl, alkenyl or alkynyl group with up to 10 carbon atoms, linear or branched, or one of the D-CnF2n + 1 groupings, where D represents an alkylene, alkenyl or alkynyl group with up to 8 carbon atoms, linearly branched, and n an integer from 1 to 8, L-CH = CF - CpF2p + 1, where L represents a C2-7 alkylene, alkenyl or alkynyl group, linear or branched, and represents an integer from 2 to 7, DO- (CH2) -q-aryl, where D represents the same as indicated, qa 0, 1, 2 or 3 and aryl appears for a phenyl or 1- or 2-naphthyl moiety, in given cases, substituted once or twice, or a heteroaryl moiety, DO- (CH2) r-CnF2n + 1, where D and n represent the same as already indicated, and figure for a whole number of 1 to 5, or R20 and R21, together with the nitrogen to which they are attached, form a saturated or unsaturated heterocycle with 5 or 6 chain members which, in given cases, contains one or two heteroatoms selected from nitrogen, oxygen and sulfur and in given cases, it is substituted or Z is shown for -SOx- and x for 0, 1 or 2, where, then, R20 represents an alkyl, alkenyl group or alkynyl with up to 10 carbon atoms, linear or branched, or one of the D-CnF2n + 1 groupings, where D represents an alkyl, alkenyl or alkynyl group with up to 8 carbon atoms, linear or branched, and an integer from 1 to 8, L - CH = CF - CpF2p + 1, where L represents a
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
DE1997158390 DE19758390A1 (en) | 1997-12-23 | 1997-12-23 | New 11beta-halo-7alpha-substituted-estratriene derivatives are useful for treatment e.g. various cancers, anovulatolial infertility, male hair loss, osteoporosis, and contraceptives |
DE1998106357 DE19806357A1 (en) | 1998-02-10 | 1998-02-10 | New 11 beta-halo-7 alpha-substituted estratrienes useful for treating e.g. estrogen-dependent disease such as breast cancer |
Publications (1)
Publication Number | Publication Date |
---|---|
AR015500A1 true AR015500A1 (en) | 2001-05-02 |
Family
ID=26042916
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP980106471A AR015500A1 (en) | 1997-12-23 | 1998-12-18 | 11 BETA-HALOGEN-STRATRIENS REPLACED IN 7 ALPHA, PROCEDURE FOR PREPARING PHARMACEUTICAL PREPARATIONS THAT CONTAIN SUCH 11 BETA-HALOGEN-STRATRIENS REPLACED IN 7 ALPHA, AS WELL AS USED IN THE PREPARATION OF MEDICINES. |
Country Status (27)
Country | Link |
---|---|
US (1) | US6780855B2 (en) |
EP (1) | EP1042355B1 (en) |
JP (1) | JP2001527088A (en) |
KR (1) | KR20010024806A (en) |
CN (1) | CN1131235C (en) |
AR (1) | AR015500A1 (en) |
AT (1) | ATE232543T1 (en) |
AU (1) | AU750801B2 (en) |
BG (1) | BG104553A (en) |
BR (1) | BR9814416A (en) |
CA (1) | CA2316444A1 (en) |
DE (1) | DE59807213D1 (en) |
DK (1) | DK1042355T3 (en) |
EA (1) | EA002623B1 (en) |
EE (1) | EE200000380A (en) |
ES (1) | ES2191371T3 (en) |
HU (1) | HUP0100568A3 (en) |
ID (1) | ID26207A (en) |
IL (1) | IL136938A0 (en) |
IS (1) | IS5526A (en) |
NO (1) | NO20003286L (en) |
NZ (1) | NZ505348A (en) |
PE (1) | PE20000129A1 (en) |
PL (1) | PL341299A1 (en) |
SK (1) | SK9442000A3 (en) |
TR (1) | TR200001973T2 (en) |
WO (1) | WO1999033855A1 (en) |
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WO2002032429A2 (en) * | 2000-10-18 | 2002-04-25 | Schering Aktiengesellschaft | Use of inhibitors of progesterone receptor for treating cancer |
AU2006202187B2 (en) * | 2001-11-27 | 2008-11-06 | Bayer Schering Pharma Aktiengesellschaft | 17alpah-alkyl-17beta-oxy-estratrienes and intermediate products for their production, uses thereof and pharmaceutical preparations |
DE10159217A1 (en) * | 2001-11-27 | 2003-06-05 | Schering Ag | 17alpha-alkyl-17ß-oxy-estratrienes and intermediates for their preparation, use of 17alpha-alkyl-17ß-oxy-estratriene for the preparation of medicaments and pharmaceutical preparations |
US20040242551A1 (en) * | 2003-05-28 | 2004-12-02 | Schering Ag | Composition comprising antiprogestins and pure antiestrogens for prophylaxis and treatment of hormone-dependent diseases |
AU2003267773A1 (en) * | 2003-10-14 | 2005-04-27 | Council Of Scientific And Industrial Research | (3r, 4r)-trans-3,4-diarylchroman derivatives with estrogenic activity |
KR20070061526A (en) * | 2004-07-27 | 2007-06-13 | 시코르, 인크. | A PROCESS FOR THE PREPARATION OF 7alpha;-ALKYLATED 19-NORSTEROIDS |
CN103121962B (en) | 2005-11-22 | 2014-11-12 | 住友化学株式会社 | Organic sulfur compounds and use thereof as arthropodicides |
DE102007023614A1 (en) | 2007-05-21 | 2008-11-27 | Bayer Schering Pharma Aktiengesellschaft | New amide compounds used for treatment of gynecological diseases e.g. endometriosis, for female fertility control and female hormone replacement therapy, has general formula |
DE102007049630A1 (en) | 2007-10-11 | 2009-10-29 | Bayer Schering Pharma Aktiengesellschaft | New amide compounds used for therapy and/or prophylaxis of gynecological diseases e.g. endometriosis, for female fertility control and female hormone replacement therapy |
JP2009001551A (en) | 2007-05-18 | 2009-01-08 | Sumitomo Chemical Co Ltd | Organic sulfur compound and its use for controlling harmful arthropod |
JP5298631B2 (en) | 2007-05-18 | 2013-09-25 | 住友化学株式会社 | Organic sulfur compounds and their use for controlling harmful arthropods |
TW200904329A (en) | 2007-05-18 | 2009-02-01 | Sumitomo Chemical Co | Organic sulfur compound and its use for controlling harmful arthropod |
DE102007032800A1 (en) | 2007-07-10 | 2009-01-15 | Bayer Schering Pharma Aktiengesellschaft | Nonsteroidal progesterone receptor modulators |
EP2033948A1 (en) * | 2007-08-30 | 2009-03-11 | Bayer Schering Pharma Aktiengesellschaft | Process for preparing Estrogen-antagonistic 11beta-Fluoro-17alpha-alkylestra-1,3,5 (10)-triene-3, 17-diols having a 7alpha-(xi-Alkylamino-omega-perfluoroalkyl)alkyl side chain and alpha-Alkyl(amino)-omega-perfluoro(alkyl)alkanes and processes for their preparation |
EP2826475B1 (en) | 2007-10-16 | 2019-03-20 | Repros Therapeutics Inc. | Trans-clomiphene for treating diabetes in hypogonadal men |
EP2053055A1 (en) * | 2007-10-24 | 2009-04-29 | Bayer Schering Pharma Aktiengesellschaft | 11.beta.-fluoro-3-acetoxyestra-3,5-diene-17-one and method for its manufacture |
DE102007058747A1 (en) | 2007-12-05 | 2009-06-10 | Bayer Schering Pharma Aktiengesellschaft | Nonsteroidal progesterone receptor modulators |
EP2070942A1 (en) | 2007-12-13 | 2009-06-17 | Bayer Schering Pharma Aktiengesellschaft | Method for aromatising 19-nor-androst-4-en-3-ones to estra-1,3,5(10)-trienes |
EP2070909A1 (en) | 2007-12-15 | 2009-06-17 | Bayer Schering Pharma AG | Non-steroidal progesterone receptor modulators |
EP2070941A1 (en) | 2007-12-14 | 2009-06-17 | Bayer Schering Pharma Aktiengesellschaft | Stereoselective synthesis of selective estrogen receptor down-regulators |
EP2258375A1 (en) | 2009-06-04 | 2010-12-08 | Bayer Schering Pharma Aktiengesellschaft | 17B-alkyl-17alpha-oxy-estratrienes |
DE102009034362A1 (en) | 2009-07-20 | 2011-01-27 | Bayer Schering Pharma Aktiengesellschaft | 17-Hydroxy-17-pentafluoroethyl-estra-4,9 (10) -diene-11-aryl derivatives, process for their preparation and their use for the treatment of diseases |
DE102009034366A1 (en) | 2009-07-20 | 2011-01-27 | Bayer Schering Pharma Aktiengesellschaft | 17-Hydroxy-17-pentafluoroethyl-estra-4,9 (10) -diene-11-methyleneoxyalkylene aryl derivatives, process for their preparation and their use for the treatment of diseases |
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KR102198059B1 (en) | 2013-04-11 | 2021-01-05 | 바이엘 파마 악티엔게젤샤프트 | Progesterone receptor antagonist dosage form |
AU2013386732B2 (en) * | 2013-04-18 | 2018-10-18 | Xi'an Libang Pharmaceutical Technology Co., Ltd. | Ester derivative of 7-alpha-[9-(4,4,5,5,5-pentafluoropentylsulphinyl)nonyl]oestra-1,3,5(10)-triene-3,17beta-diol having antitumour activity and preparation method thereof |
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CN106146599A (en) * | 2015-04-07 | 2016-11-23 | 江苏希迪制药有限公司 | A kind of recovery is because of the method for sulfoxide configuration ratio underproof fulvestrant or derivatives thereof |
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US3076829A (en) * | 1961-09-15 | 1963-02-05 | Schering Corp | Novel 9, 11-disubstituted estratriene derivatives |
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DE19635525A1 (en) * | 1996-08-20 | 1998-02-26 | Schering Ag | New 7-alpha-(xi-aminoalkyl)- oestratriene derivatives |
-
1998
- 1998-12-18 AR ARP980106471A patent/AR015500A1/en not_active Application Discontinuation
- 1998-12-18 PE PE1998001246A patent/PE20000129A1/en not_active Application Discontinuation
- 1998-12-23 IL IL13693898A patent/IL136938A0/en unknown
- 1998-12-23 CN CN98812631A patent/CN1131235C/en not_active Expired - Fee Related
- 1998-12-23 KR KR1020007006955A patent/KR20010024806A/en not_active Application Discontinuation
- 1998-12-23 AT AT98966410T patent/ATE232543T1/en not_active IP Right Cessation
- 1998-12-23 TR TR2000/01973T patent/TR200001973T2/en unknown
- 1998-12-23 HU HU0100568A patent/HUP0100568A3/en unknown
- 1998-12-23 EP EP98966410A patent/EP1042355B1/en not_active Expired - Lifetime
- 1998-12-23 NZ NZ505348A patent/NZ505348A/en unknown
- 1998-12-23 DE DE59807213T patent/DE59807213D1/en not_active Expired - Fee Related
- 1998-12-23 PL PL98341299A patent/PL341299A1/en unknown
- 1998-12-23 AU AU22763/99A patent/AU750801B2/en not_active Ceased
- 1998-12-23 DK DK98966410T patent/DK1042355T3/en active
- 1998-12-23 EA EA200000711A patent/EA002623B1/en not_active IP Right Cessation
- 1998-12-23 SK SK944-2000A patent/SK9442000A3/en unknown
- 1998-12-23 US US09/380,413 patent/US6780855B2/en not_active Expired - Fee Related
- 1998-12-23 ES ES98966410T patent/ES2191371T3/en not_active Expired - Lifetime
- 1998-12-23 WO PCT/EP1998/008470 patent/WO1999033855A1/en not_active Application Discontinuation
- 1998-12-23 EE EEP200000380A patent/EE200000380A/en unknown
- 1998-12-23 CA CA002316444A patent/CA2316444A1/en not_active Abandoned
- 1998-12-23 BR BR9814416-2A patent/BR9814416A/en not_active IP Right Cessation
- 1998-12-23 ID IDW20001234A patent/ID26207A/en unknown
- 1998-12-23 JP JP2000526531A patent/JP2001527088A/en active Pending
-
2000
- 2000-06-09 IS IS5526A patent/IS5526A/en unknown
- 2000-06-22 NO NO20003286A patent/NO20003286L/en not_active Application Discontinuation
- 2000-06-23 BG BG104553A patent/BG104553A/en unknown
Also Published As
Publication number | Publication date |
---|---|
ATE232543T1 (en) | 2003-02-15 |
NO20003286D0 (en) | 2000-06-22 |
CN1131235C (en) | 2003-12-17 |
DE59807213D1 (en) | 2003-03-20 |
EA002623B1 (en) | 2002-06-27 |
NZ505348A (en) | 2002-10-25 |
HUP0100568A3 (en) | 2002-01-28 |
CA2316444A1 (en) | 1999-07-08 |
EP1042355B1 (en) | 2003-02-12 |
JP2001527088A (en) | 2001-12-25 |
CN1286693A (en) | 2001-03-07 |
DK1042355T3 (en) | 2003-04-22 |
ID26207A (en) | 2000-12-07 |
EP1042355A1 (en) | 2000-10-11 |
WO1999033855A1 (en) | 1999-07-08 |
AU2276399A (en) | 1999-07-19 |
EE200000380A (en) | 2001-12-17 |
SK9442000A3 (en) | 2001-04-09 |
PL341299A1 (en) | 2001-04-09 |
ES2191371T3 (en) | 2003-09-01 |
KR20010024806A (en) | 2001-03-26 |
NO20003286L (en) | 2000-08-23 |
IL136938A0 (en) | 2001-06-14 |
EA200000711A1 (en) | 2001-02-26 |
IS5526A (en) | 2000-06-09 |
US20030069434A1 (en) | 2003-04-10 |
BR9814416A (en) | 2000-10-10 |
BG104553A (en) | 2001-02-28 |
TR200001973T2 (en) | 2001-01-22 |
PE20000129A1 (en) | 2000-03-11 |
AU750801B2 (en) | 2002-07-25 |
US6780855B2 (en) | 2004-08-24 |
HUP0100568A2 (en) | 2001-08-28 |
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